| 摘要 |
PURPOSE: Novel aromatic amidine derivatives having a potent and selective thrombine inhibitory activity, process for preparing the same and composition for thrombine inhibition containing the same as an active ingredient are provided which may be administered orally. CONSTITUTION: A compound of formula (I), pharmaceutically acceptable salt and stereochemical isomer are provided. In formula, A represents C2 to C6 alkylene capable being substituted by C1 to C4 alkyl, halogeno C1 to C4 alkyl, C1 to C4 alkoxyl C1 to C4 alkyl, hydroxy C1 to C4 alkyl; R1 represents H, or C1 to C4 alkyl capable being substituted by C1 to C4 alkyl or phenyl; R2 and R3 represent each independently H, each carboxyl, halogen, carbamoyl, amino, methylsulfonylamino, C1 to C4 alkylamino, di(C1 to C4 alkyl)amino, hydroxy, C1 to C4 alkyl or C1 to C5 alkanoyl capable being mono- or multi-substituted by C1 to C4 alkoxycarbonyl or C1 to C4 alkoxycarbamoyl.
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